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WO/2014/047391A1 |
Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein. Also disclosed are methods of using such compounds to inhibit the Not...
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WO/2014/047374A1 |
Disclosed are compounds of Formula (I) and/or salts thereof: (I) wherein: R1 is CH2CH2CF3; R2 is CH2(cyclopropyl), CH(CH3)(cyclopropyl), or CH2CH2CH3; R3 is H, CH3, or Rx; R4 is H or Ry; and Rx, Ry, Ra, Rb, Rc, y, and z are defined herei...
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WO/2014/047372A1 |
Disclosed are compounds of Formula (I) and/or salts thereof: (I) wherein R1 is CH2CH2CF3; R2 is CH2CH2CF3 or CH2CH2CH2CF3; R3 is H, CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein...
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WO/2014/037313A1 |
The invention relates to the use of substituted benzodiazepinones and benzazepinones of general formula (I) or the salts thereof, the groups in general formula (I) corresponding to the definitions cited in the description, for increasing...
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WO/2014/026997A1 |
What are described are BET protein-inhibitory, in particular BRD4-inhibitory, 2,3-benzodiazepines of the general formula (I) in which R1a, R1b, R1c, R2, R3, R4, R5, A and X have the meanings given in the description, intermediates for pr...
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WO/2013/167177A1 |
The present invention relates to chemical compounds acting through GPR17 receptor for use in the treatment of diseases, in particular for use in chronic and/or acute neurodegenerative diseases, preferably Multiple Sclerosis, inflammatory...
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WO/2013/161993A1 |
The present invention pertains to: a novel trans-2-decenoic acid derivative or a pharmaceutically acceptable salt thereof; and a drug containing the compound as the active ingredient. Specifically, the trans-2-decenoic acid derivative or...
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WO/2013/135750A1 |
The present invention relates to a new class of diazepine-derivatives as chel ating agents for paramag netic metal ions, the process for their preparation, and use of such paramagnetic complexes as contrast agents, particularly suitable ...
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WO/2013/126797A1 |
Conjugates are described herein where CCK2R targeting ligands are attached to an active moiety, such as therapeutic agent or an imaging agent, through a linker. The conjugates can be used in the detection, diagnosis, imaging and treatmen...
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WO/2013/123217A1 |
A method of administering an oligonucleotide of interest into a cell (e.g., a mammalian cell) is carried out by concurrently administering an intracellular trafficking route inhibitor to the cell in an amount effective to increase the de...
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WO/2013/110134A1 |
The present invention relates to heterocyclic compounds useful for antagonising angiotensin II Type 2 (AT2) receptor. More particularly the invention relates to piperazine and diazepine compounds, compositions containing them and their u...
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WO/2013/105608A1 |
The present invention relates to a diazepine derivative represented by general formula (I) (In the formula: R1 and R2 are a hydrogen atom, etc. or R1 and R2 together with a benzene ring to which they are attached are a naphthalene ring, ...
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WO/2013/096560A1 |
Methods and compositions for producing formulations for orally inhaled benzodiazepines that do not require the presence of a surface modifier are described. The formulations are useful in the treatment of epileptic seizures.
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WO/2013/068785A1 |
The invention relates to indanone/indandione derivatives and heterocyclic analogs of Formula (I) wherein Ar1, A, B, L1, Y, Z, and (R1)n n are as described in the description; to pharmaceutically acceptable salts thereof, and to the use o...
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WO/2013/064231A1 |
The invention provides modulators for the orphan nuclear receptor RORγ and methods for treating RORγ mediated diseases by administration of these novel RORγ modulators to a human or a mammal in need thereof. Specifically, the present ...
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WO/2013/033246A9 |
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WO/2013/028382A1 |
Compounds having the structure of Formula Ia, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing ather...
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WO/2013/006485A1 |
The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the c...
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WO/2011/100838A9 |
Compounds of formula (I) wherein m, R1, R2, R3, X and Y are defined herein, are useful as inhibitors of HIV replication.
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WO/2012/176878A1 |
[Problem] To provide a novel proteasome inhibitor which can be administered orally. [Solution] A proteasome inhibitor comprising, as an active ingredient, a compound represented by general formula (1) [wherein Y and Y' are the same as or...
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WO/2012/148553A1 |
The present invention is directed to processes for preparing a diazepane compound which is an antagonist of orexin receptors, and which is useful in the treatment or prevention of neurological and psychiatric disorders and diseases in wh...
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WO/2012/129353A1 |
Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is CH2CF3 or CH2CH2CF3; R2 is CH2CF3, CH2CH2CF3, or CH2CH2CH2CF3; R3 is H or CH3; each Ra is independently F, Cl, -CN, -OCH3, and/or NHCH2CH2OCH3; and z is zero, 1, ...
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WO/2012/124696A1 |
[Problem] To provide a compound which is useful as an active ingredient of a pharmaceutical composition, especially of a pharmaceutical composition for the prophylaxis and/or treatment of VAP-1 associated diseases. [Solution] As a result...
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WO/2012/115608A2 |
Disclosed herein are methods for treating a disease involving α-synucleic aggregation using (1) a compound which reduces the amount of polyamines in an amount effective to reduce α-synucleic aggregation; (2) a compound which inhibits p...
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WO/2012/097682A1 |
The present invention relates to compounds of formula (1) or pharmaceutical acceptable salts, wherein R1, X, Y, Z, A, B, G1, and n are defined in the description. The present invention relates also to compositions containing said compoun...
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WO/2012/031090A9 |
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WO/2012/072620A1 |
The present invention describes compounds of formula (I), and in particular the 7- nitro-5-phenyl-1 -(pyrrolidin-1 -ylmethyl)-1 H-benzo[e][1,4]diazepin-2(3H)-one compound and their pharmaceuticall acceptable salts. The compounds of the i...
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WO/2012/064483A1 |
A transamination process is described to prepare polyamine product mixtures from reactants comprising mixed nitrogen-containing compounds with binary carbon spacing between nitrogen-containing groups (a binary component). A second nitrog...
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WO/2012/059432A1 |
The present invention relates to N-Phenyl-(homo)piperazinyl-benzenesulfonyl or benzenesulfonamide compounds of formula I wherein the variables have the meanings given in the claims and the description, pharmaceutical compositions contain...
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WO/2012/045194A1 |
Disclosed are compounds which inhibit the activity of focal adhesion kinase, compositions containing the compounds, and methods of treating diseases during which focal adhesion kinase is expressed.
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WO/2012/040258A2 |
The invention includes a compound of formula I... wherein R1, Y, A, n, R4 and Z have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise th...
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WO/2012/036253A1 |
A heterocyclic compound represented by the general formula (1) or a salt thereof: wherein m, l, and n respectively represent an integer of 1 or 2; X represents -O- or -CH2-; R1 represents hydrogen, a lower alkyl group, a hydroxy-lower al...
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WO/2012/035549A2 |
The present invention is related to an improved process and intermediate(s) for the synthesis of beta amino acid derivatives of formula (I). The compounds of formula I act as DPP-IV inhibitors and are useful in the treatment of Type 2 di...
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WO/2012/008478A1 |
A diazepine derivative represented by the general formula (III) (In the formula: R21 and R22 independently represent a hydrogen atom, C1-8 alkyl group or the like; R23 represents a hydrogen atom, C1-8 alkyl group or the like; R24 and R25...
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WO/2011/151652A1 |
The invention concerns benzodiazepine derivatives of Formula (I): wherein X, L1, L2, R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined in the description. The present invention also relates to processes for the preparation of such com...
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WO/2011/123536A1 |
The present invention is directed to a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The variables for Structural Formula (I) are defined herein. Also described is a pharmaceutical composit...
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WO/2011/118672A1 |
Disclosed is a pharmaceutical product, particularly a pharmaceutical composition having a plasma kallikrein inhibition activity and is useful as a prophylactic or therapeutic agent for edemas (particularly hereditary vascular edema and c...
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WO/2011/107474A1 |
The instant invention relates to derivatives of formula (I) and their application in therapeutics.
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WO/2011/078413A1 |
Provided is a compound that has a nitrogen-containing seven-membered ring skeleton represented by formula (I) and is useful in the prevention or treatment of pathological conditions in which chymase is involved. Also provided is a drug, ...
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WO/2011/072174A1 |
Compounds and compositions comprising compounds useful in the treatment of cancer are described herein. The compounds and compositions can be used to modulate an isocitrate dehydrogenase (IDH) mutant (e.g., IDHIm or IDH2m) having alpha h...
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WO/2011/067219A1 |
Compounds of the Formula (I), wherein m, n, X1, X2, Y1, Y2, R1 and R2 are as defined herein. Also provided are pharmaceutical compositions, methods of using, and methods of preparing the compounds.
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WO/2011/048032A1 |
The invention is concerned with novel bicyclic compounds of Formula (I), wherein n, m, p, A, L, R1, R2, R3, R4, R5, R6, R7, R7, R8, R9 and R10 are as defined in the description and in the claims, as well as physiologically acceptable sal...
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WO/2011/000945A9 |
An aminoalkarnide of the formula I for use as a medicament to treat inflammatory, degenerative or demyelinating diseases of the CNS in a subject in need thereof.
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WO/2011/036204A1 |
The invention relates to a novel class of [1,4]-benzodiazepine derivatives, processes for their preparation, intermediates usable in these processes, and pharmaceutical compositions containing the compounds. Other aspects of the inventio...
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WO/2011/034078A1 |
Disclosed is a compound which is useful as the active ingredient of a medicinal composition, in particular, a medicinal composition for preventing and/or treating a VAP-1 associated disease. As the results of intensive studies on compoun...
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WO/2011/027156A1 |
The invention concerns benzodiazepine derivatives of Formula (I) wherein W, X, L1, L2, L3, R1, R2, R3, R4, R5, R6 and R7 are as defined in the description. The present invention also relates to processes for the preparation of such compo...
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WO/2011/021676A1 |
Provided is a process for industrially advantageously, easily, and efficiently producing a key intermediate for a benzo[b][1,4]diazepine-2,4-dione compound that is a therapeutic agent for arrhythmia. The process is for producing a compou...
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WO/2011/021726A2 |
The present invention provides a novel diazepine compound that blocks the IKur current or the Kv1.5 channel potently and more selectively than other K+ channels. The present invention relates to a diazepine compound represented by Genera...
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WO/2011/001928A1 |
Provided is a Michael addition reaction product of a specific compound having groups that function as a Michael donor and a monomer or polymer having groups that function as a Michael acceptor. Also provided are a photoinitiator comprisi...
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WO/2010/125135A1 |
The present invention relates to novel benzenesulfonanilide compounds of the formulae I and I' and physiologically tolerated acid addition salts and the N-oxides thereof. The compounds possess valuable therapeutic properties and are part...
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